Tryptophan dendrimers that inhibit HIV replication, prevent virus entry and bind to the HIV envelope glycoproteins gp120 and gp41

被引：25

作者：

Rivero-Buceta, Eva ^{[1
]}

Doyagueez, Elisa G. ^{[1
]}

Colomer, Ignacio ^{[1
]}

Quesada, Ernesto ^{[1
]}

Mathys, Leen ^{[2
]}

Noppen, Sam ^{[2
]}

Liekens, Sandra ^{[2
]}

Camarasa, Maria-Jose ^{[1
]}

Perez-Perez, Maria-Jesus ^{[1
]}

Balzarini, Jan ^{[2
]}

San-Felix, Ana ^{[1
]}

机构：

[1] Inst Quim Med IQM CSIC, Madrid 28006, Spain

[2] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Leuven, Belgium

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2015年 / 106卷

关键词：

Antiviral agents; AIDS; HIV; Tryptophan; HUMAN-IMMUNODEFICIENCY-VIRUS; DRUG DEVELOPMENT; IN-VITRO; INFECTION; THERAPY; TARGET; ENFUVIRTIDE; DERIVATIVES; DISCOVERY; POTENT;

D O I：

10.1016/j.ejmech.2015.10.031

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Dendrimers containing from 9 to 18 tryptophan residues at the peryphery have been efficiently synthesized and tested against HIV replication. These compounds inhibit an early step of the replicative cycle of HIV, presumably virus entry into its target cell. Our data suggest that HIV inhibition can be achieved by the preferred interaction of the compounds herein described with glycoproteins gp120 and gp41 of the HIV envelope preventing interaction between HIV and the (co)receptors present on the host cells. The results obtained so far indicate that 9 tryptophan residues on the periphery are sufficient for efficient gp120/gp41 binding and anti-HIV activity. (C) 2015 Elsevier Masson SAS. All rights reserved.

引用

页码：34 / 43

页数：10

共 52 条

[1] Synthesis, Langmuir and Langmuir-Blodgett film behaviour of new dendritic amphiphiles [J].